[CAS NO. 905281-76-7] GDC-0879
PRODUCTS SPECIFICATIONS [905281-76-7]
DESCRIPTION [905281-76-7]
Overview
| MDL | MFCD16875916 |
|---|---|
| Molecular Weight | 334.37 |
| Molecular Formula | C19H18N4O2 |
| SMILES | O/N=C1C(C=CC(C2=CN(CCO)N=C2C3=CC=NC=C3)=C4)=C4CC/1 |
3 Publications Citing Use of MCE
Summary
GDC-0879 is a potent and selective B-Raf inhibitor with an IC 50 of 0.13 nM.
IC50 & Target
|
B-Raf 0.13 nM (IC 50 ) |
In Vitro
GDC-0879 also inhibits pERK with an IC 50 of 63 nM [1] . GDC-0879 represents a novel potent and selective B-Raf inhibitor that is being evaluated as a potential antitumor agent. GDC-0879 exhibits potent inhibition of Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines with low cellular pMEK1 inhibition IC 50 estimates of 59 and 29 nM in A375 melanoma and Colo205 colorectal carcinoma cells, respectively [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The pharmacokinetic parameters of GDC-0879 after oral administration of 15, 25, 50, 100, and 200 mg/kg in MCT in mice are estimated as follows: k a =8.20 h -1 , k e =0.59 h -1 , and apparent volume of distribution=6.19 L/kg [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 149.53 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9907 mL | 14.9535 mL | 29.9070 mL |
| 5 mM | 0.5981 mL | 2.9907 mL | 5.9814 mL |
| 10 mM | 0.2991 mL | 1.4953 mL | 2.9907 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.48 mM); Clear solution
References
- [1] Hansen JD, et al. Potent and selective pyrazole-based inhibitors of B-Raf kinase. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5.
- [2] Wong H, et al. Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations,